Synthesis of New Pyrazole Derivatives, Their Anti-Inflammatory and Analgesic Activities, and Molecular Docking Studies


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Abstract

A new series of coupled benzofuran derivatives that contain the trifluoromethyl group and pyrazole moiety is synthesized for evaluation of their anti-inflammatory and analgesic activities. Their synthesis proceeds via cyclocondensation of 2-hydroxy-4-(trifluoromethyl)benzaldehyde with chloroacetone with formation of 2-acetylbenzofuran, which upon treatment with different aldehydes via the Claisen-Schmidt condensation gives the corresponding chalcones. Cyclization of chalcones with hydrazine hydrate leads to pyrazoline derivatives, that exhibit significant anti-inflammatory and analgesic activities. Docking modelling of selected active compounds are correlated well with their anti-inflammatory tests data.

About the authors

M. F. El Shehry

Pesticide Chemistry Department; Al-Zahrawi University College

Email: ewiesfawzy@yahoo.com
Egypt, Giza, 12622; Karbala

E. F. Ewies

Organometallic and Organometalloid Chemistry Department

Author for correspondence.
Email: ewiesfawzy@yahoo.com
Egypt, Giza, 12622

E. M. Zayed

Green Chemistry Department

Email: ewiesfawzy@yahoo.com
Egypt, 33 El-Bohouth St. (former El Tahrir St.), Dokki, Giza, 12622

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